Safinamide

Catalog No.S5357 Batch:S535701

Print

Technical Data

Formula

C17H19FN2O2
Molecular Weight 302.34 CAS No. 133865-89-1
Solubility (25°C)* In vitro DMSO 60 mg/mL (198.45 mM)
 
 
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Safinamide (EMD-1195686, PNU-15774E) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.
Targets
MAO-B [1]
(Microsomal)
16.7 nM(Ki)
In vitro The antiparkinson mechanism of safinamide is through reversible inhibition of selective MAO-B, thus reducing the degradation of dopamine. It inhibits glutamate release and dopamine reuptake in the brain. Safinamide also blocks sodium and calcium channels[2].
In vivo Safinamide is absorbed quickly, with a bioavailability of 95%, and a demonstrated time to maximum plasma concentration of 1.8-2.8 hours. It exhibits extensive extravascular distribution with a volume of distribution of approximately 165 L. Safinamide does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. Safinamide is mediated by cytochrome P450 (CYP) 3A4 isoenzymes. It is 88% to 90% plasma protein-bound and is primarily eliminated through the kidneys (approximately 76%) in the form of its metabolites, with an elimination half-life of 20 to 30 hours. About 1.5% of safinamide is found excreted in the feces. Safinamide exhibits linear pharmacokinetics after oral administration of 50 mg to 300 mg (three times the maximum recommended daily dose) with a steady state reached within five to six days[2].

Protocol (from reference)

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.